In the current study, we investigated the inhibitory activity of pyridoxine, pyridoxal,\nand pyridoxamine, against various digestive enzymes such as �±-glucosidases, sucrase, maltase,\nand glucoamylase. Inhibition of these enzymes involved in the absorption of disaccharide can\nimprove post-prandial hyperglycemia due to a carbohydrate-based diet. Pyridoxal (4.14 mg/mL\nof IC50) had the highest rat intestinal �±-glucosidase inhibitory activity, followed by pyridoxamine\nand pyridoxine (4.85 and 5.02 mg/mL of IC50, respectively). Pyridoxal demonstrated superior\ninhibition against maltase (0.38 mg/mL IC50) and glucoamylase (0.27 mg/mLIC50). In addition,\npyridoxal showed significant higher �±-amylase inhibitory activity (10.87 mg/mL of IC50) than that of\npyridoxine (23.18 mg/mL of IC50). This indicates that pyridoxal can also inhibit starch hydrolyzing by\npancreatic �±-amylase in small intestine. Based on these in vitro results, the deeper evaluation of the\nanti-hyperglycemic potential of pyridoxine and its derivatives using Sprague-Dawley (SD) rat models,\nwas initiated. The post-prandial blood glucose levels were tested two hours after sucrose/starch\nadministration, with and without pyridoxine and its derivatives. In the animal trial, pyridoxal\n(p < 0.05) had a significantly reduction to the postprandial glucose levels, when compared to the\ncontrol. The maximum blood glucose levels (Cmax) of pyridoxal administration group were decreased\nby about 18% (from 199.52 �± 22.93 to 164.10 �± 10.27, p < 0.05) and 19% (from 216.92 �± 12.46 to\n175.36 �± 10.84, p < 0.05) in sucrose and starch loading tests, respectively, when compared to the control\nin pharmacodynamics study. The pyridoxal administration significantly decreased the minimum,\nmaximum, and mean level of post-prandial blood glucose at 0.5 h after meals. These results indicate\nthat water-soluble vitamin pyridoxine and its derivatives can decrease blood glucose level via the\ninhibition of carbohydrate-hydrolyzing and absorption-linked enzymes. Therefore, pyridoxal may\nhave the potential to be used as a food ingredient for the prevention of prediabetes progression to\ntype 2 diabetes.
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